Zeta Potential Research Articles

Investigation of Folate-Functionalized Magnetic-Gold Nanoparticles Based Targeted Drug Delivery for Liver: In Vitro, In Vivo and Docking Studies.

Magnetic nanoparticles used for targeted drug administration present a promising approach in cancer treatment owing to its notable advantages, such as targeted and enhanced encapsulation ability and improved bio protection compared with conventional drug delivery methods. Au shell-iron core nanoparticles (Fe3O4@Au) were manufactured by a chemical process, coated with dextran to encapsulate curcumin, and functionalized for precision drug delivery using folic acid to combat liver cancer. Dynamic light scattering, scanning electron microscopy, transmission electron microscopy, vibrational spectroscopy, and magnetometry were applied to assess the synthesis of the Fe3O4@Au-DEX-CU-FA compound. The mean size, zeta potential, and polydispersity of Fe3O4@Au-DEX-CU-FA were 63.3 ± 2.33 nm, -68.3 ± 1.78 mV, and 0.041 ± 0.008, respectively. Molecular docking models were created to examine the relationship between Fe3O4@Au-CU and BCL-XL, BAK, and to identify potential binding sites. The loading efficiency and release profile tests examined the medication delivery system's ability. MTT assay was subsequently utilized to determine the optimal dosage and therapeutic efficacy of Fe3O4@Au-DEX-CU-FA on cancer SNU-449 and healthy THLE-2 cell lines. Flow cytometry demonstrated that Fe3O4@Au-DEX-CU-FA effectively induced cancer cell death. Fe3O4@Au-DEX-FA showed a regulated release profile of free curcumin at 37 °C and pH values of 7.4 and 5.4. Real-time PCR revealed increased BAK expression and decreased BCL-XL expression. Nude tumor-bearing mice were used for in vivo experiments. Fe3O4@Au-DEX-CU-FA treatment dramatically reduced the swelling size compared with free CU and control treatments. It also resulted in a longer lifespan, expanded splenocyte proliferation, increased IFN-γ levels, and decreased IL-4 levels. The regular cells showed no cytotoxic effect compared with the cancer type, confirming that Fe3O4@Au-DEX-CU-FA maintained its potent anticancer actions. The data suggests that Fe3O4@Au-DEX-CU-FA possesses a promising potential as a therapeutic agent for combating tumors.

Pharmaceutical Applications and Advances with Zetasizer: An Essential Analytical Tool for Size and Zeta Potential Analysis

Abstract: Zetasizer is an advanced device that measures various properties of particles or molecules suspended in a liquid medium. It is extensively used for evaluating the size of nanoparticles, colloids, and biomolecular particles, and for determining particle charge. There are several analytical techniques by which the size, zeta potential, and molecular weight can be determined, like Dynamic Light Scattering (DLS) that measures the size of particles in dispersed systems, which can range from sub-nanometers to several micrometers in diameter. Electrophoretic Light Scattering (ELS) analyzes the mobility and charge of particles, also known as the zeta potential. Static Light Scattering (SLS) determines the molecular weight of particles in a solution. The Zetasizer is part of the Zetasizer Advance range of benchtop systems available for laboratory use. The Zetasizer Ultra model offers unique measurement capabilities, such as Multi-angle Dynamic Light Scattering (MADLS) and particle concentration. These features offer a deeper understanding of samples, making the Zetasizer a vital instrument in numerous scientific and industrial applications. In this review, we have discussed Zetasizer’s principles for the determination of particle size, zeta potential, and molecular weight, along with its qualification and applications in different formulations.

Synthesis and Characterization of Gold Nanoparticles and Gold Nanoparticles Loaded with Bromelain

The production and use of nanometallic elements, such as gold, have received a lot of attention lately due to their distinctive features and wide range of uses. Most of these studies have employed the Turkevich approach. This research employed the Turkevich technique to produce gold nanoparticles (AuNPs). AuNPs and bromelain-loaded AuNPs were characterised using a variety of methods, including ultraviolet-visible spectroscopy (UV-Vis), Fourier transform infrared spectroscopy (FTIR), field emission scanning electron microscopy (FE-SEM), X-ray diffraction (XRD), transmission electron microscopy (TEM), and zeta potential (ZP) measurements. The UV-Vis spectra of Bromelain, AuNPs, and AuNPs-Bromelain each had a peak at 276, 534, and 550 nm wavelengths, respectively. The FE-SEM and TEM studies revealed the presence of spherical particles with a smooth surface. The diameters of the AuNPs ranged from 49.32 to 77.29 nm; the diameters of the Bromelain-AuNPs ranged from 46.39 to 75.66 nm, as determined by the FE-SEM analysis. The TEM analysis indicated that the particles' sizes ranged from 7.40 to 15 nm for AuNPs and 14.51 nm for AuNPs-Bromelain. The XRD patterns revealed numerous diffraction peaks, indicating the crystal structure of the synthesised nanoparticles. FTIR spectrometry was employed to identify the functional groups in the synthesised nanoparticles. Zeta potential (ZP) measurements revealed that AuNPs had a zeta potential value of +0.1±0.4, and the zeta potential value for AuNPs-Bromelain was +1.2±3.0 mV.

Formulation Design and Characterization of Nilotinib Polymeric Nanoparticles by Nanoprecipitation Technique for the Improved Drug Solubility and Dissolution Rate

Introduction: Nilotinib is a BCS class-IV poorly water-soluble kinase inhibitor drug, that was used for this study to prepare the polymeric nanoparticles by nanoprecipitation technique using Eudragit RL-100 and RS-100 as polymers, Killophore P-188 as a surfactant, and PEG 400 used as a non-volatile, and nontoxic solvent for the improvement of the drug solubility and dissolution rate. Method: The initial process and formulation variables are screened out based on the selected critical quality attributes such as drug release (%), particle size (nm), zeta potential (mV), and polydispersity index. The FT-IR and DSC studies reveal that the drug has no compatibility between the selected drug and the polymers and does not show any additional drug peaks after physical mixing and formulations. The prepared nanoparticles were further characterized to evaluate the particle size (nm), polydispersity index (PDI), zeta potential (mV), entrapment efficiency (%), and in-vitro drug release (%). From the in vitro drug release study, Eudragit RL-100 and Killophore P-188-based formulations showed optimum drug entrapment efficiency with improved drug solubility and dissolution rate in PEG 400 compared to Eudragit RS-100-based formulations. The accelerated stability data for the optimized formulation batch (F6) before and after storage conditions at 40±2 0C and 75±5% RH indicates that the optimized formulation (F6) is more stable for up to 6 months without changes in drug entrapment efficiency and in vitro dissolution rate. Dissolution kinetic data and diffusion exponent values suggested that optimized formulation followed the Higuchi model with a non-Fickian transport mechanism. Result: According to the results, the preparation method proposed in this study is the most suitable for generating polymeric nanoparticles of nilotinib for improved drug solubility and dissolution rate. Conclusion: The nilotinib-based polymeric nano-formulation proved a potential alternative for better drug release with an enhanced solubility rate.

Green Synthesis of CuO Nanoparticles Mediated Rhazya Stricta Plant Leaves Extract Characterization and Evaluation of their Antibacterial and Anticancer Activity (in vitro Study)

In this study, a straightforward, expeditious, and environmentally friendly approach to synthesize copper oxide nanoparticles (CuONPs) utilizing an aqueous extract of Rhazya Stricta (R. stricta) leaves was employed. The CuONPs underwent various analytical techniques for characterization, including X-ray diffractometer (XRD), field emission scan electron microscope (FESEM), energy dispersive X-ray (EDX) analyses, UV-Vis spectroscopy, Fourier transform infrared spectroscopy (FTIR), and zeta potential. The XRD analysis authenticated the monoclinic crystal nature, revealing an average crystallite size of 15.6 nm. FESEM images depicted semi-spherical and cubic shapes, with particle sizes ranging from 56.64 to 86.95 nm. The formation of CuONPs was initially confirmed by the observable change in colour, attributed to the excitation of surface Plasmon resonance at 280 nm in the UV-Vis spectra. FTIR analysis affirmed the presence of functional groups in the R. Stricta leaves extract, serving as both reducing and stabilizing agents, facilitating the formation of CuONPs. Zeta potential measurements indicated substantial stability with a value of 46.6 mV. The biosynthesized CuONPs were further evaluated for their antibacterial properties against Klebsiella Pneumoniae (K. pneumoniae) and Staphylococcus aureus (S. aureus), yielding inhibition zones of 21 mm and 30 mm, respectively. Additionally, the cytotoxicity assessment of CuONPs against A549 cell lines revealed higher cytotoxicity of 81.47 ± 1.517 at a CuONP concentration of 100 μg/ml. This work is the first attempt at R. stricta-facilitated synthesis of CuONPs as antibacterial and anticancer agents. It can subsequently be exploited as a potential candidate for these agents and might be utilized further in vivo studies.

Synthesis, Evaluation, and Biocompatibility Study of Magnetite Nano Particles in Normal Cells and Cancer Cells for Health Care Application

Magnetic nanoparticles have been synthesized in a very simple and economical way by the co-precipitation method, where the effect of molar concentrations of ferric chloride anhydrous (FeCl3) and iron (II) sulphate heptahydrate (FeSO4.7H20) on magnetite synthesis has been investigated. Also, a detailed study was conducted to study the effect of magnetite and hematite on both normal and cancerous cell lines. After this, the magnetic nanoparticles obtained were analyzed by x-ray Diffraction (XRD), scanning electron microscope (SEM) - energy dispersive x-ray (EDX), Fourier transform infrared spectroscopy (FTIR), zeta potential, vibrating sample magnetometer (VSM), atomic force microscopy (AFM), MTT test, and cell apoptotic assay. The XRD peaks for magnetite were easily discernible in the final formulation. SEM images showed round particles in nano ranges, and FTIR peaks showed the presence of magnetite. Zeta potential showed surface charges. VSM showed the magnetic property of magnetite, and AFM confirmed SEM images. It can be concluded that magnetic nanoparticles were synthesized by the co-precipitation method using an optimized molar concentration of reagents. Also, the necessity of coating uncoated magnetic nanoparticles can be seen from the MTT assay. Cell apoptotic assays have shown that synthesized magnetite nanoparticles have shown potential apoptotic activity on cancer cell lines.

A multi-component paclitaxel −loaded β-elemene nanoemulsion by transferrin modification enhances anti-non-small-cell lung cancer treatment

A multi-component paclitaxel (PTX) −loaded β-elemene nanoemulsion by transferrin modification (Tf-PE-MEs) was developed to enhance non-small-cell lung cancer (NSCLC) treatment. After transferrin modification, the particle size of Tf-PE-MEs was (14.87 ± 1.84) nm, and the zeta potential was (−10.19 ± 0.870) mV, respectively. In vitro experiments showed that Tf-PE-MEs induced massive apoptosis in A549 cells, indicating that it had significant cytotoxicity to A549 cells. Through transferrin modification, Tf-PE-MEs accumulated at the tumor site efficiently with overexpressed transferrin receptor (TfR) on the surface of A549 cells. This will allow increasing PTX and β-elemene concentration in the target cells, enhancing the therapeutic effect. Compared to PTX alone, Tf-PE-MEs displayed good anti-tumor efficacy and diminished systemic toxicity in vivo studies. With favourable therapeutic potential, this study provides a new strategy for the combined anticancer treatment of non-small cell lung cancer.

On-line enrichment and separation of glycoprotein by capillary electrophoresis based on pH response coating column

A capillary column coated with 3-aminophenylboronic acid (APBA)-functionalized gold nanoparticles (AuNPs@APBA) was prepared via electrostatic self-assembly. The coated column exhibited anti-nonspecific adsorption of glycoproteins, enabling selective online enrichment during capillary electrophoresis (CE). First, gold nanoparticles (AuNPs) were synthesized using the sodium citrate reduction method. Then, APBA was self-assembled electrostatically on the surface of the AuNPs to obtain AuNPs@APBA. This nanomaterial was bonded to the inner wall of a capillary through ion adsorption to produce a AuNPs@APBA-coated capillary column. Glycoproteins were adsorbed via bond formation with boric acid groups under alkaline conditions (pH 8) to generate borate esters. Under acidic conditions (pH 3), the borate esters dissociated to release the glycoproteins, thereby achieving the selective online enrichment and separation of glycoproteins. The AuNPs and AuNPs@APBA were characterized using Fourier transform infrared spectroscopy, and their sizes and Zeta potentials were determined. In addition, the electroosmotic flow (EOF) of the AuNPs@APBA-coated capillary column was measured. The results showed that the surface of the AuNPs was successfully modified with APBA and that AuNPs@APBA was adsorbed on the inner wall of the capillary. The peak area of ovalbumin (OVA) on the AuNPs@APBA-coated column was 26.46 times higher than that on a bare column via conventional electrophoresis. In contrast, the peak area of bovine serum albumin (BSA) only increased by 8.47 times, indicating that the AuNPs@APBA coated column selectively enriched glycoproteins. Evaluation of the reproducibility and stability of this method revealed that the AuNPs@APBA coated capillary column could be used continually for 33-67 h. The relative standard deviations (RSDs) of the peak areas for intra-day (n=5) and inter-day (n=6) analyses were 2.2% and 3.0%, respectively. The developed method was successfully applied to enrich glycoproteins in a 1×106-fold diluted egg white sample. Glycoproteins were not detected using conventional electrophoresis on the bare column, whereas the AuNPs@APBA-coated capillary column effectively enriched and separated glycoproteins, resulting in a peak area of 10469 mAU·ms. Furthermore, the entire enrichment and separation process was completed within 3 min. This new online enrichment and separation method for glycoproteins has the advantages of low sample consumption, simple operation, and high separation efficiency.

Characteristics and modification mechanism of recycled waste silty clay slurry as the shield slag conditioner

The construction process of earth pressure balance shield (EPBS) generates a large amount of shield slag. In China, the conventional methods for treating shield slag involve crude landfill and stockpiling, resulting in increased cost and significant environmental issues. To expand the recycling of shield slag, this study proposes to use waste silty clay to completely replace bentonite as a conditioner in coarse-grained strata. Firstly, the physical properties of silty clay slurries are investigated with four additives. There are six modified silty clay slurries with good improved performance. Then, analyzing the rheological properties of six modified silty clay slurries, and verifying the feasibility of replacing bentonite slurry with modified silty clay slurry. Next, scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR) and Zeta potential were used to analyse the micromechanisms, molecular structures and molecular forces of 14% bentonite slurry, silty clay slurry with a soil-water ratio of 1:1, sodium carbonate 3% and sodium silicate 0.1% in a silty clay slurry with a soil-water ratio of 1:1. Finally, the slump test was carried out to verify the improvement effect of the modified silty clay slurry on the shield slag. The results show that sodium carbonate modified silty clay slurry has a higher interlayer water content and greater ion exchange capacity. When the soil-water ratio is 1:1 and the concentration of sodium carbonate is 3%, the apparent viscosity and shear force of the modified silty clay slurries are between those of bentonite slurries with a concentration of 10% and 14%. Additionally, the modified silty clay slurry showed a stable microstructure and good residue amendment effect, making it suitable as a soil conditioner during EPBS construction in coarse-grained strata. This study offers a viable approach for recycling EPBS slurry.

Recycled ionic liquid vs. deep eutectic solvent in cellulose nanocrystals production: characterization, techno-economic analysis, and life cycle assessment

Three scenarios involving aqueous mixtures of neoteric solvents have been evaluated as solvents and catalysts for the cellulose hydrolysis reaction to obtain CNC in high yields (>70%). The scenarios considered were: scenario 1 (S1) involves a recyclable ionic liquid dilution of [Hmim][(HSO4)(H2SO4)]/H2O (64 wt% IL); scenario 2 (S2) another recyclable dilution of [Hmim][(HSO4)(H2SO4)]//H2O (80 wt% IL) and scenario 3 (S3) a non-recyclable ternary deep eutectic solvent (60 wt% DES: choline chloride: oxalic acid/30 wt% PA/10 wt% water). Experimental analysis, techno-economic, and life cycle analysis (LCA) indicate that S1 emerges as a suitable scenario among the three analyzed. S1 demonstrated the highest competitiveness, with a lower raw material cost per gram of CNC produced (US$0.81/g) and lower environmental contributions concerning climate change and fossil fuel depletion, accounting mainly for its recyclability. Therefore, the recyclable dilution of 64 wt% IL used in S1 appears to be the most viable option for sustainable and environmentally conscious CNC production. Besides, the physicochemical properties of the CNC were revealed: aspect ratio range 7-8, high dispersion stability related to zeta potential > -40 mV, good crystallinity range 50-80%, and thermal stability with Tonset> 300 °C. These results guided towards a scenario with crucial advantages: a diluted IL that retains its acidity after reuse cycles by a facile recovery process, maintaining high CNC production performance and providing low environmental impacts.

Antioxidant, In Vitro Cytotoxicity, and Anti-diabetic Attributes of a Drug-Free Guar Gum Nanoformulation as a Novel Candidate for Diabetic Wound Healing.

The escalating intersection of diabetes and impaired wound healing poses a substantial societal burden, marked by an increasing prevalence of chronic wounds. Diabetic individuals struggle with hindered recovery, attributed to compromised blood circulation and diminished immune function, resulting in prolonged healing periods and elevated healthcare expenditures. To address this challenge, we report here a drug-free novel guar gum (GG)-based nano-formulation which is effective against diabetic wound healing. Nanoparticles with an average particle size of 32.4nm display stability with negative zeta potential. Differential scanning calorimetry (DSC) and Fourier transform infrared (FTIR) analysis reveal alterations in thermal properties and molecular structures induced by the nano-particulation process. In vitro studies highlight the antioxidant potential of GGNP through concentration-dependent free radical scavenging activity in DPPH and ABTS assays. The nanoformulation also exhibits inhibitory effects on α-glucosidase and α-amylase enzymes. Cell viability studies have indicated moderate cytotoxicity in L929 cells and significant proliferation and migration in HaCaT cells, suggesting a positive impact on skin cells. In vitro enzymatic activity assessments under hyperglycaemic conditions reveal the potential of GGNP to modulate glutathione-S-transferase (GST), superoxide dismutase (SOD), and catalase activities as well as decreasing lipid peroxidation (LPO) levels, showcasing an antioxidant response. These results suggest GGNP as a promising candidate in diabetic wound healing.

Evaluating the operational properties of concrete admixtures containing molecularly modified polycarboxylate superplasticizers.

The objective of this study focused on the design and preparation of a molecularly modified polycarboxylate superplasticizer to develop concretes with enhanced engineering features. For this purpose, polyethylene glycol was chemically modified with maleic anhydride to give the mono polyethylene glycol maleate (MPEGM). Then, polycarboxylate superplasticizer comprising of isoprenyl oxy polyethylene glycol (TPEG) and acrylic acid (AA, PCE-1), and the synthesized MPEGM with TPEG and AA (PCE-2) were prepared through solution radical polymerization. Subsequently, concrete mixtures with different dosages (0, 0.1, 0.15, 0.2, 0.25, 0.3wt%) of PCE-1 and PCE-2 were prepared. Chemical structure of the synthesized MPEGM and superplasticizers together with their copolymer composition were identified by FTIR and 1HNMR analyses. The molecular weights (Mw) and molecular weight distributions (PDI) of PCE-1 (8.74 × 104, 1.36) and PCE-2 (8.74 × 104, 2.19) were studied by GPC analysis, respectively. The zeta potential of cement particles (2.8mV) becomes negative in the presence of 0.6g/L of PCE-1 (- 7.8) and PCE-2 (- 9.5). This implies that electrostatic and steric hindrance forces of adsorbed superplasticizers synergistically provide a situation for appropriate dispersion of cement particles. The results of water-reducing percentage, fluidity, air content, bleeding water rate, initial and final setting times, wet density, flexural and compressive properties, and ultrasonic pulse velocity analyses exhibit significant enhancement on the features of concrete mixtures made of polycarboxylate superplasticizer. The superiority of PCE-2 to PCE-1 was connected to its adsorption-dispersibility potent induced by stronger electrostatic and steric repulsion forces, which result in quality and continuity enhancement in concretes.

Preparation of magnetite nanoparticles and their application in the removal of methylene blue dye from wastewater.

Wastewater is discharged in large amounts from different industries; thus, wastewater treatment is currently one of the main concerns, advanced oxidation is a promising technique for wastewater treatment. This research aims to synthesize magnetite nanoparticles and study their application in wastewater treatment via adsorption and advanced oxidation processes. Magnetite nanoparticles were synthesized via coprecipitation technique between ferric and ferrous sulfate at a molar ratio of 2:1. The prepared sample was characterized using FTIR, XRD, TEM, BET surface area, zeta potential, VSM, and UV‒visible spectroscopy. XRD confirmed the formation of a single face-centered cubic (FCC) spinel structure of Fe3O4. TEM revealed an average particle size of 29.2nm and a BET surface area of 70.1 m2g-1. UV‒visible spectroscopy revealed that the UV-visible peak of the sample was obtained at 410nm. VSM confirmed the attraction of the sample to a magnet with a magnetization of 60(emu/g). The removal efficiency of methylene blue was studied using adsorption and advanced oxidation methods. For adsorption, the studied parameters were dye concentration 2-10ppm, 3-10pH, and 50:300mg Fe3O4/L. For advanced oxidation, peroxide was used with nanomagnetite as a catalyst, and the studied parameters were pH 2-11, magnetite dose 20-200PPM, and peroxide dose 500-2000PPM. The removal efficiency by adsorption reached 95.11% by adding 50 mg of Fe3O4/L and 10 ppm dye conc at 6.5 pH; on the other hand, in advanced oxidation, it reached 98.5% by adding 110PPM magnetite and 2000ppm H2O2 at pH 11. The magnetite nanoparticles were reused for ten cycles of advanced oxidation, for a 10% reduction in removal efficiency at the tenth cycle.

Enhanced catalytic performance of Candida rugosa lipase through immobilization on zirconium-2-methylimidazole: A novel biocatalyst approach.

Immobilization of enzymes on suitable supports is a critical approach for enhancing enzyme stability, reusability, and overall catalytic efficiency. This study explores the immobilization of Candida rugosa lipase on zirconium-based 2-methylimidazole (ZrMI) nanoparticles, aiming to develop a stable and reusable biocatalyst. The ZrMI was produced via a solvothermal technique and analyzed using various characterization methods. Candida rugose lipase was immobilized using cross-linking agents, achieving an 87 % immobilization efficiency. The immobilized enzyme exhibited significantly enhanced thermal stability, broader pH tolerance, and increased catalytic efficiency compared to free C. rugose lipase. The ZrMI@lipase retained 69 % of its enzymatic activity following a 60-day storage period at 4 °C. Notably, it displayed significant reusability, maintaining 65 % of its original activity after undergoing 15 catalytic cycles. Examination of the kinetics revealed that the immobilized enzyme possessed a heightened substrate affinity (Km of 4.1 mM) and maximal reaction rate (Vmax of 85.7 μmol/mL/min) in comparison to the free enzyme (Km of 5.4 mM and Vmax of 69 μmol/mL/min), indicating enhanced catalytic efficiency. Validation through zeta potential and hydrodynamic size assessments verified the successful binding of the enzyme and the consistent colloidal characteristics. These results suggest that ZrMI is a promising support for C. rugose lipase immobilization, offering improved stability and reusability for various industrial applications. The study highlights the potential of ZrMI@lipase as an efficient and durable biocatalyst, contributing to advancements in enzyme immobilization technology and sustainable industrial processes.

Preparation and Optimization of Beta-Sitosterol Nanosuspension-Loaded In situ Gel by Using Box-Behnken Model for the Treatment of Prostate Cancer

Introduction: Prostate cancer is the second most often occurring cancer in males and the fourth most common cancer overall. Beta-sitosterol (β-Sit), the most prevalent plant phytosterol found in several plant species, has been reported to have inhibitory effects against several malignancies. Even though β-Sit has considerable potential, its therapeutic uses are limited due to its poor aqueous solubility (<0.1mg/ml), low bioavailability (0.41%), and poor absorption from GIT. Nanosuspension is one of the most innovative approaches to address problems linked to low solubility and poor absorption. Method: In the present research work, β-Sit nanosuspension has been fabricated by nanoprecipitation- ultrasonication, followed by high-pressure homogenization (Panda plus 2000) employing HPMC E5 and poloxamer (188 and 407) as stabilizers, optimized using a Box-Behnken technique. Subsequently, in situ nano gel was prepared by dispersion method using gellan gum as an ionsensitive polymer by incorporating optimized nanosuspension. Results: The optimized nanosuspension was evaluated for various parameters and has been found to have an average particle size (137 ± 5.07 nm), zeta potential (-24±4.99), PDI (0.207), and improved solubility up to 5 folds, being suitable for systemic absorption through the nasal route. The optimized in situ gel was characterized and showed the desired viscosity, good spreadability, acceptable gelation property, and sufficient mucoadhesive strength to adhere to nasal mucosa after ionic interaction. The in vitro release of pure drug, nanosuspension, and the optimized gel was compared, and optimized in situ gel showed a maximum release of 91.41 ± 1.32% up to 8 hours. Conclusion: It was concluded that the in situ nasal nanogel could be the best possible approach to delivering β-Sit into systemic circulation for the treatment of prostate cancer.

Development and optimization of a self micro-emulsifying drug delivery system (SMEDDS) for co-administration of sorafenib and curcumin.

In this study, we developed a novel co-administration of curcumin and sorafenib using a Self micro-emulsifying Drug Delivery System (SMEDDS) called Sorafenib-Curcumin Self micro-emulsifying Drug Delivery System (SOR-CUR-SMEDDS). The formulation was optimized using star point design-response surface methodology, and in vitro cellular experiments were conducted to evaluate the delivery ratio and anti-tumor efficacy of the curcumin and sorafenib combination. The SOR-CUR-SMEDDS exhibited a small size distribution of 13.48 ± 0.61nm, low polydispersity index (PDI) of 0.228 ± 0.05, and negative zeta potential (ZP) of - 12.4 mV. The half maximal inhibitory concentration (IC50) of the SOR-CUR-SMEDDS was 3-fold lower for curcumin and 5-fold lower for sorafenib against HepG2 cells (human hepatocellular carcinoma cells). Transmission electron microscopy (TEM) and particle size detection confirmed that the SOR-CUR-SMEDDS droplets were uniformly round and within the nano-emulsion particle size range of 10-20nm. The SMEDDS were characterized then studied for drug release in vitro via dialysis membranes. Curcumin was released more completely in the combined delivery system, showing the largest in vitro drug release (79.20%) within 7 days in the medium, while the cumulative release rate of sorafenib in the release medium was low, reaching 58.96% on the 7day. In vitro pharmacokinetic study, it demonstrated a significant increase in oral bioavailability of sorafenib (1239.88-fold) and curcumin (3.64-fold) when administered in the SMEDDS. These findings suggest that the SMEDDS formulation can greatly enhance drug solubility, improve drug absorption and prolong circulation in vivo, leading to increased oral bioavailability of sorafenib and curcumin.

Post-calcination as an effective approach to enhance adsorption of arsenic and antimony anions by Mg/Al layered double hydroxide-decorated spent coffee ground biochars: Role of charge properties and active sites

This study evaluated the effects of post-calcination on the charge properties and active sites of Mg/Al layered double hydroxide-decorated spent coffee ground biochars (LDHMgAl@SCGB) governing adsorption behaviors and mechanisms of arsenic (AsV) and antimony (SbV) anions from aqueous phases. Post-calcinated LDHMgAl@SCGB (PLDHMgAl@SCGB) exhibited higher adsorption capacities for AsV and SbV compared to spent coffee ground biochars (SCGB) and LDHMgAl@SCGB as post-calcination of LDHMgAl@SCGB enhanced the charge properties (surface zeta potential at pH 7.0: SCGB = –21.8 mV, LDHMgAl@SCGB = 28.5 mV, and PLDHMgAl@SCGB = 34.4 mV) and increased active sites by eliminating the anions (i.e., Cl- ions) and water molecules at its interlayers. The calculated kinetic, intra-particle diffusion, and isotherm parameters indicated that the chemisorption and intra-particle diffusion were mainly responsible for the adsorption of AsV and SbV by SCGB, LDHMgAl@SCGB, and PLDHMgAl@SCGB. Moreover, post-calcination of LDHMgAl@SCGB enhanced its selectivity toward AsV and SbV by reinforcing the electrostatic surface complexation via its improvement of charge properties. Since PLDHMgAl@SCGB exhibited the excellent reusability for the adsorption of AsV (reuse efficiency > 63.6%) and SbV (reuse efficiency > 52.1%), it can be concluded that post-calcination of LDHMgAl@SCGB is a promising method for improving the adsorption capacities for AsV and SbV in real water matrices.

Design of experiment (DoE) of mucoadhesive valproic acid-loaded nanostructured lipid carriers (NLC) for potential nose-to-brain application

Epilepsy is a highly prevalent neurological disease and valproic acid (VPA) is used as a first-line chronic treatment. However, this drug has poor oral bioavailability, which requires the administration of high doses, resulting in adverse effects. Alternative routes of VPA administration have therefore been investigated, such as the nose-to-brain route, which allows the drug to be transported directly from the nasal cavity to the brain. Here, the use of nanostructured lipid carriers (NLC) to encapsulate drugs administered in the nasal cavity has proved advantageous. The aim of this work was to optimise a mucoadhesive formulation of VPA-loaded NLC for intranasal administration to improve the treatment of epilepsy. The Design of Experiment (DoE) was used to optimise the formulation, starting with component optimisation using Mixture Design (MD), followed by optimisation of the manufacturing process parameters using Central Composite Design (CCD).The optimised VPA-loaded NLC had a particle size of 76,1 ± 2,8 nm, a polydispersity index of 0,190 ± 0,027, a zeta potential of 28,1 ± 2,0 mV and an encapsulation efficiency of 85,4 ± 0,8%. The in vitro release study showed VPA release from the NLC of 50 % after 6 h and 100 % after 24 h. The in vitro biocompatibility experiments in various cell lines have shown that the optimised VPA-loaded NLC formulation is safe up to 75 µg/mL, in neuronal (SHSY5Y), nasal (RPMI) and hepatic (HepG2) cells. Finally, the interaction of the optimised VPA-loaded NLC formulation with nasal mucus was investigated and mucoadhesive properties were observed. The results of this study suggest that the use of intranasal VPA-loaded NLC may be a promising alternative to promote VPA targeting to the brain, thereby improving bioavailability and minimising adverse effects.

Multifunctional targeting of docetaxel plus bakuchiol micelles in the treatment of invasion and metastasis of ovarian cancer.

The invasion and metastasis of tumors pose significant challenges in the treatment of ovarian cancer (OC), making it difficult to cure. One potential treatment approach that has gained attention is the use of matrix metalloproteinase (MMP) reactive controlled release micelle preparations. In this study, we developed a novel PEG5000-PVGLIG-hyaluronic acid docetaxel/bakuchiol (PP-HA-DTX/BAK) micelles formulation with desirable characteristics such as particle size, narrow PDI, and a ZETA potential of approximately -5mV. The surface modification with HA facilitates tumor penetration into the tumor interior, while the incorporation of DSPE-PEG2000-PVGLIG-PEG5000 helps conceal DSPE-PEG2000-HA, reducing off-target effects and prolonging drug circulation time in vivo. Both in vitro and in vivo experiments demonstrated that these micelles effectively inhibit proliferation, invasion, and metastasis of OC cells while promoting apoptosis. Therefore, our findings suggest that PP-HA-DTX/BAK micelles represent a safe and effective therapeutic strategy for treating OC.

Hansen solubility parameters and quality-by-design oriented optimized cationic nanoemulsion for transdermal drug delivery of tolterodine tartrate.

Tolterodine tartrate (TOT) is a selective anti-muscarinic drug to treat urinary urgency and overactive urinary bladder (OAB) occurring in children, renal disease and elderly patients. Oral delivery is associated with several adverse effects. We addressed HSPiP and QbD (quality by design)-oriented TOT loaded cationic nanoemulsions for transdermal delivery. Hansen solubility parameters (HSP) screened excipients based on theoretical solubility whereas, QbD optimized cationic nanoemulsions (CNE-TOT-6). Formulation characteristic parameters were desirable to execute targeted in vitro drug release and ex vivo permeation profiles. In vitro hemolysis was conducted at varied concentrations whereas, histopathological study supported the safety aspect of CNE-TOT6. A comparative bioavailability was carried out in a rat model. Capmul PG8 (CAP), tween 80, and PEG 400 (polyethylene glycol 400) were screened based on HSP and experimental solubility data. QbD suggested optimized content of CAP, tween 80, and PEG 400 to achieve the lowest value of size (184 nm), maximum % entrapment efficiency (87.2 %), high zeta potential (+32.6 mV), optimum viscosity (47.19 cP), and high extrudability (96 %) as compared to its gel. High gel consistency slowed down the drug release and permeation flux as compared to CNE-TOT6 suspension. Hemocompatible CNE-TOT6 increased pharmacokinetic parameters as compared to the control and gel without causing skin toxicity after application. Thus, HSPiP and QbD oriented cationic nanoemulsions are promising carriers to treat overactive urinary bladder.